Physicochemical Characterisation of Polysaccharides from the Seeds and Leaves of Miracle Fruit (Synsepalum dulcificum) and Their Antioxidant and α-Glucosidase Inhibitory Activities In Vitro

Miracle fruit (Synsepalum dulcificum) has been well known and studied for its unique taste-modifying ability. In this study, the monosaccharide composition, molecular weight (Mw), and in vitro bioactivities (antioxidant, α-glucosidase inhibition) of polysaccharides from the seeds (MFP-S) and leaves (MFP-L) of miracle fruit were investigated. The results showed that MFP-S was a homogeneous polysaccharide (Mw 2804 Da) with glucose. MFP-L displayed three fractions (92093, 1496, and 237 Da) consisting of rhamnose, arabinose, galactose, glucose, and xylose. Moreover, the antioxidant and α-glucosidase inhibition of MFP-L were significantly greater than those of MFP-S. The α-glucosidase inhibition of MFP-L was remarkably better than the positive control, acarbose (an antidiabetes drug). More specifically, the 50% inhibitory concentration (IC50) values of α-glucosidase activities for MFP-S, MFP-L, and acarbose were 33, 0.01, and 1 mg mL−1, separately. Therefore, MFP-L can be developed as a functional factor with both antioxidant and antidiabetes activities in food applications.

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Pentagamavunon-0 (PGV-0) Enhance Cytotoxic Effect of Doxorubicin through Increasing of Apoptosis, Senescence and ROS Level on Triple Negative Breast Cancer 4T1

Indonesian Journal of Cancer Chemoprevention ◽

10.14499/indonesianjcanchemoprev11iss1pp7-15 ◽

2020 ◽

Vol 11 (1) ◽

pp. 7

Author(s):

Ismanurrahman Hadi ◽

Riris Istighfari Jenie ◽

Edy Meiyanto

Keyword(s):

Combination Treatment ◽

In Vitro Model ◽

Annexin V ◽

Positive Control ◽

Breast Cancers ◽

Single Treatment ◽

Ic50 Values ◽

Vitro Model ◽

Better Than

TNBC, one of the sub type of breast cancers was widely known with high tumorigenic and poor prognosis than others. The development of combination agent (co-chemotherapy) with doxorubicin for chemotherapy of TNBC were carried out to decrease doxorubicin side effect and resistance in cancer. This present study aims to explore the co-chemotherapeutic properties of PGV-0 and investigate induction of doxorubicin on apoptosis, senescence and ROS against TNBC. 4T1 Cell line were used as a TNBC in vitro model. Cytotoxic measurement was performed using MTT assay resulting in IC50 values of 52 μM. Meanwhile, the combination of doxorubicin and PGV-0 showed synergistic effect which decreased cell viability of 4T1 better than single treatment of doxorubicin. Apoptosis analysis was performed using annexin V/PI assay indicated that the combination treatment of PGV-0 and doxorubicin increased apoptosis evidence. Senescence detection was carried out using senescence-associated-β galactosidase (SA-β-gal) assay. The results showed that a single treatment of PGV-0 induced cellular senescence and increased senescence cells in combination treatment. Moreover, DCFDA staining showed that PGV-0 increased ROS level at single treatment, whereas combination treatment increased ROS intracellular compared to the positive control of doxorubicin. Based on these results, PGV-0 has potential as a co-chemotherapeutic candidate on TNBC.Keyword: 4T1, PGV-0, Co-chemotherapy, Cytotoxic, Senescence, Apoptosis, ROS

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Two new compounds from leaves of Bruguiera cylindrica (L.) Blume with the in vitro α-glucosidase inhibitory activity

Science and Technology Development Journal ◽

10.32508/stdj.v23i4.2457 ◽

2021 ◽

Vol 23 (4) ◽

Author(s):

Thuy Thi Le Nguyen ◽

Tung Thanh Bui ◽

Phung Kim Phi Nguyen ◽

Chi Minh Tran ◽

Tu Dang Cam Phan ◽

...

Keyword(s):

Inhibitory Activity ◽

Ethyl Acetate Extract ◽

Chemical Constituents ◽

Positive Control ◽

Chemical Structures ◽

Ic50 Values ◽

Bruguiera Cylindrica ◽

New Compounds ◽

Better Than

Introduction: Bruguiera cylindrica is one of the mangrove plants belonging to Bruguiera genus. This genus is characterized by the presence of a large number of compounds, but the research on bioactivities has not been investigated so far. In the present research, the α-glucosidase inhibitory activity, as well as chemical constituents of the ethyl acetate extract of this plant, were studied. Methods: The chemical structures of two new compounds were elucidated by spectroscopic and computational methods. Results: Two new compounds, benzobrugierol (1) and bruguierine (2), were isolated from leaves of Bruguiera cylindrica (L.) Blume, together with nine known ones, including lupeol (3), betulin (4), chrysoeriol (5), glut-5-ene-3-ol (6), cholesta-4-ene-3-one (7), 3α-(Z)-coumaroyllupeol (8), 3α-(E)-coumaroyllupeol (9), 3β-hydroxycholesta-5-ene-7-one (10) and β-sitosterol 3-O-β-D-glucopyranoside (11). Extracts and some isolated compounds were evaluated for α-glucosidase inhibitory activities. Conclusion: The results showed that most of the extracts and tested compounds exhibited activities better than the positive control acarbose, especially two new compounds 1 and 2 with their IC50 values of 17.9 ± 0.4 and 34.6 ± 0.7 (mg/mL), respectively.

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Synthesis and biological activity of aldehyde derivatives of isopimaric acid

Letters in Organic Chemistry ◽

10.2174/1570178618666210813121953 ◽

2021 ◽

Vol 18 ◽

Author(s):

Yanju Lu ◽

Zhendong Zhao ◽

Yuxiang Chen ◽

Jing Wang

Keyword(s):

Inhibitory Concentration ◽

Inhibitory Effect ◽

Positive Control ◽

Klebsiella Pneumonia ◽

Hep G2 ◽

Isopimaric Acid ◽

Streptococcus Pneumonia ◽

Derivatives Of ◽

Better Than

: Four series of acylhydrazone derivatives, including halogenated aryl modified acylhydrazone, thiophene, pyrrole and quinoline, were synthesized and characterized. The minimum inhibitory concentrations of the compounds against five bacteria were determined and most of the compounds displayed some degree of antibacterial activity. Isopimaric acid (pyrrole-3-carboxaldehyde) acylhydrazone (3j) exhibited the most potent activity against Streptococcus pneumonia and Klebsiella Pneumonia, with the minimum inhibitory concentration being 3.91 μg/mL. The antimicrobial activity against S. pneumoniae was improved when the pyrrole structure was introduced into isopimaric acid. All heterocyclic acylhydrazone derivatives of isopimaric acid exhibited a good in vitro antitumorial activity at 100 μM. It is concluded that the inhibitory effect of isopimaric acid (2-fluoro-6-methoxybenzaldehyde) acylhydrazone (3d) on Hep G2 and isopimaric acid (3-bromothiophene-2-carbaldehyde) acylhydrazone (3g) on Hep G2 and MDAMB 231 is better than that of the positive control 5-fluorouracil (5-FU) (76.51%), which is a widely used clinical anticancer agent, at 100 μM.

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Synthesis and Activity of New Schiff Bases of Furocoumarin

Heterocyclic Communications ◽

10.1515/hc-2020-0115 ◽

2020 ◽

Vol 26 (1) ◽

pp. 176-184

Author(s):

Huijun Xie ◽

Chao Niu ◽

Zeyang Chao ◽

Nuramina Mamat ◽

Haji Akber Aisa

Keyword(s):

Animal Models ◽

Amphotericin B ◽

Molecular Mechanism ◽

Schiff Bases ◽

Positive Control ◽

Excellent Performance ◽

Activation Rate ◽

Antibacterial Spectrum ◽

Better Than

AbstractFurocoumarins, such as 8-MOP, are the most common medications used to relieve the symptoms of vitiligo clinically. Some furocoumarins also showed excellent performance in an anti-bacterial assay. This paper describes the synthesis of a series of novel Schiff bases (6a-6k), and their promotion in melanogenesis and anti-bacterial properties were studied in vitro.The pigment production of B16 cells and bacterial inhibition ring assay were applied for the bioactivity of 6a-6k. According to the results, a stronger promotion on pigment content was observed, when six compounds co-cultured with cells, compared with positive control (8-MOP). Significantly, compound 6k (237%) as the most active was found to increase the amount of melanin more than 1.7 times compared with 8-MOP activation rate (136%). All the compounds could moderately retard C. albicans growth. Interestingly, aldehyde 5, which possessed a broader antibacterial spectrum, showed the highest inhibition against C. albicans as well and much better than the positive control (Amphotericin B).Studies of 6k in animal models of vitiligo and related molecular mechanism are presently under way, with the aim of discovering an anti-vitiligo leading compound.

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In Vitro α-Glucosidase and α-Amylase Inhibitory Activities of Free and Bound Phenolic Extracts from the Bran and Kernel Fractions of Five Sorghum Grain Genotypes

Foods ◽

10.3390/foods9091301 ◽

2020 ◽

Vol 9 (9) ◽

pp. 1301

Author(s):

Yun Xiong ◽

Ken Ng ◽

Pangzhen Zhang ◽

Robyn Dorothy Warner ◽

Shuibao Shen ◽

...

Keyword(s):

Digestive System ◽

Inhibitory Concentration ◽

Inhibitory Effect ◽

Inhibitory Effects ◽

Phenolic Contents ◽

Inhibitory Activities ◽

Sorghum Grain ◽

Global Health Challenge ◽

Phenolic Extracts

Diabetes is a global health challenge. Currently, an effective treatment for diabetes is to reduce the postprandial hyperglycaemia by inhibiting the carbohydrate hydrolysing enzymes in the digestive system. In this study, we investigated the in vitro α-glucosidase and α-amylase inhibitory effects of free and bound phenolic extracts, from the bran and kernel fractions of five sorghum grain genotypes. The results showed that the inhibitory effect of sorghum phenolic extracts depended on the phenolic concentration and composition. Sorghum with higher phenolic contents generally had higher inhibitory activity. Among the tested extracts, the brown sorghum (IS131C)-bran-free extract (BR-bran-free, half-maximal inhibitory concentration (IC50) = 18 ± 11 mg sorghum/mL) showed the strongest inhibition against α-glucosidase which was comparable to that of acarbose (IC50 = 1.39 ± 0.23 mg acarbose/mL). The red sorghum (Mr-Buster)-kernel-bound extract (RM-kernel-bound, IC50 = 160 ± 12 mg sorghum/mL) was the most potent in inhibiting α-amylase but was much weaker compared to acarbose (IC50 = 0.50 ± 0.03 mg acarbose/mL).

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Reduction in the in vitro sensitivity oF Drechslera tritici-repentis, isolated from wheat, to strobilurin and triazole fungicides

Summa Phytopathologica ◽

10.1590/0100-5405/2160 ◽

2017 ◽

Vol 43 (1) ◽

pp. 20-25

Author(s):

Rosane Baldiga Tonin ◽

Erlei Melo Reis ◽

Aveline Avozani

Keyword(s):

Inhibitory Concentration ◽

In Vitro Sensitivity ◽

Randomized Design ◽

Inhibition Data ◽

Ic50 Values ◽

Control Failure ◽

Quinone Outside Inhibitors ◽

Completely Randomized Design

ABSTRACT Reports of failure in the chemical control of wheat yellow leaf spot led to determination of the sensitivity of Drechslera tritici-repentis (Dtr) to the fungicides quinone outside inhibitors (QoIs) and demethylation inhibitors (DMIs). The IC50 was obtained for strobilurins (azoxystrobin, kresoxim-methyl, picoxystrobin and pyraclostrobin) and for triazoles (cyproconazole, epoxiconazole, propiconazole, prothioconazole and tebuconazole), using five Dtr isolates. Seven concentrations of the fungicides were tested in the bioassay: 0.00; 0.01; 0.10; 1.00; 10:00 and 20.00 and 40.00 mg/L active ingredient (a.i.). Assays consisted of completely randomized design and four replicates. Each experiment was performed twice, using the average of the two tests for statistical analysis. The percentage inhibition data for conidial germination (QoIs) and for mycelial growth (DMIs) were subjected to logarithmic regression analysis, calculating the 50% inhibitory concentration (IC50) based on the generated equation. There was a reduction in the sensitivity of Dtr isolates to strobilurins. IC50 values ranged from 0.58 to > 40.00 mg/L. The lowest sensitivity of isolates was detected for azoxystrobin, kresoxim-methyl, picoxystrobin and trifloxystrobin. Pyraclostrobin was most efficient, showing IC50 between 0.58 and 1.03 mg/L. The IC50 ranged from 0.35 to 1.37 mg/L for epoxiconazole, from 0.49 to 1.28 mg/L for propiconazole and from 1.41 to 2.34 mg/L for tebuconazole. Prothioconazole was most potent, showing IC50 between 0.09 and 0.21 mg/L. The hypothesis that the control failure can be attributed to the reduced Dtr sensitivity to the fungicides QoIs and DMIs was confirmed.

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DIFFERENCE BETWEEN ANTIMICROBIAL EFFECTS OF PAPACARIE AND PAPAIN ON STREPTOCOCCUS MUTANS IN VITRO

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019.v11s1.ar186 ◽

2019 ◽

pp. 79-83

Author(s):

TITTY SULIANTI ◽

NILAKESUMA DJAUHARI ◽

BAMBANG NURSASONGKO

Keyword(s):

Inhibitory Concentration ◽

Minimum Bactericidal Concentration ◽

Zone Of Inhibition ◽

Antimicrobial Effects ◽

Treatment Groups ◽

Group Control ◽

Caries Removal ◽

And Diffusion ◽

Better Than

Objective: The aim is to compare the antimicrobial effects of papain and Papacarie with dilution and diffusion tests.Methods: There were two treatment groups and one Group control. The treatment group received papain and Papacarie, and the control groupreceived chlorhexidine, in five liquids with different concentrations of 0.5%, 0.25%, 0.125%, 0.0625%, and 0.03%. The dilution and diffusion testswere used to determine the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and zone of inhibition for eachtreatment material.Results: MICs of papain and Papacarie were 12.5%, indicating that at a concentration of 12.5%, the material can inhibit the growth of Streptococcusmutans. Papain does not have an MBC value but the Papacarie has an MBC at 25%, which indicating that at a concentration of 25%, Papacarie hasbactericidal effects on S. mutans. The zone of inhibition of papain was lower than Papacarie.Conclusion: Based on chemomechanical caries removal materials, the antimicrobial effects of Papacarie were better than those of papain.

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Homoadamantane and Adamantane Acylphloroglucinols from Hypericum hirsutum

Planta Medica ◽

10.1055/a-1617-7573 ◽

2021 ◽

Author(s):

Julianna Max ◽

Jörg Heilmann

Keyword(s):

Petroleum Ether Extract ◽

2D Nmr ◽

Positive Control ◽

Ionization Mass ◽

2D Nmr Spectroscopy ◽

Vitro Assay ◽

Ionization Mass Spectroscopy ◽

Ic50 Values ◽

Adamantane Skeleton

Abstract 1H NMR-guided fractionation of the petroleum ether extract of the aerial parts from Hypericum hirsutum yielded to the isolation of 19 polyprenylated polycyclic acylphloroglucinols. Structure elucidation based on 1D and 2D NMR spectroscopy together with high-resolution electrospray ionization mass spectroscopy revealed 14 acylphloroglucinols with a homoadamantane scaffold (1–14), while 5 further compounds showed an adamantane skeleton (15–19). Except for hookerione C (15), all isolated metabolites are hitherto unknown. While structurally-related metabolites have been isolated from other Hypericum species, it is the first report of admantan and homoadamantan type acylphloroglucinols in section Taeniocarpium Jaub. & Spach (Hypericaceae). The isolated compounds have been tested in a crystal violet-based in vitro assay on their properties to reduce the proliferation of human microvascular endothelial cells compared to hyperforin as the positive control. They showed a moderate reduction of proliferation with IC50 values in the range ~ 3 – 22 µM, with the homoadamantane-based compounds 2 and 4 being the most active. In addition, inhibition of the TNF-α-induced ICAM-1 expression was determined for 1 – 5, 7, and 10 – 12. Substances 3 and 12 reduced the ICAM-1 expression significantly (to 46.7% of control for 3, 62.3% for 12, at 50 µM).

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Anti-Inflammatory Cembrane-Type Diterpenoids and Prostaglandins from Soft Coral Lobophytum sarcophytoides

Marine Drugs ◽

10.3390/md17080481 ◽

2019 ◽

Vol 17 (8) ◽

pp. 481 ◽

Cited By ~ 2

Author(s):

Hongjie Shen ◽

Xiaowan Liu ◽

Minghua Jiang ◽

Guangyuan Luo ◽

Zhenger Wu ◽

...

Keyword(s):

Nitric Oxide ◽

Mass Spectrometry ◽

Soft Coral ◽

High Resolution Mass Spectrometry ◽

Positive Control ◽

Ic50 Values ◽

Anti Inflammatory ◽

Modified Mosher’S Method ◽

Resolution Mass ◽

Better Than

Two new cembrane-type diterpenoids, lobophytins A (1) and B (3), and four new prostaglandins, (5E)-PGB2 (10), (5E)-13,14-dihydro-PGB2 (11), 13,14-dihydro-PGB2 (12) and 13,14-dihydro-PGB2-Me (13), together with ten known compounds were isolated from the soft coral Lobophytum sarcophytoides. The structures of these new secondary metabolites were identified by high resolution mass spectrometry (HR-ESIMS), nuclear magnetic resonance (NMR) and electron circular dichroism (ECD) analyses, as well as the modified Mosher’s method. Compounds 6, 7, 9, 10, 12, 13, 15 and 16 showed potential anti-inflammatory activity by inhibiting the production of nitric oxide (NO) in RAW264.7 cells that were activated by lipopolysaccharide, with IC50 values ranging from 7.1 to 32.1 μM and were better than the positive control indomethacin, IC50 = 39.8 μM.

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Potential Application of Prunus armeniaca L. and P. domestica L. Leaf Essential Oils as Antioxidant and of Cholinesterases Inhibitors

Antioxidants ◽

10.3390/antiox8010002 ◽

2018 ◽

Vol 8 (1) ◽

pp. 2 ◽

Cited By ~ 5

Author(s):

Marco Bonesi ◽

Maria Tenuta ◽

Monica Loizzo ◽

Vincenzo Sicari ◽

Rosa Tundis

Keyword(s):

Gas Chromatography ◽

Essential Oils ◽

Antioxidant Properties ◽

Positive Control ◽

Prunus Armeniaca ◽

Gas Chromatography Mass Spectrometry ◽

Flame Ionization ◽

Ic50 Values ◽

Comprehensive Comparison

The aim of this work is to investigate the in vitro acetylcholinesterase (AChE) and butyrycholinesterase (BChE) inhibitory activities of essential oils obtained by hydrodistillation from the leaves of Prunus armeniaca and P. domestica in relation to their composition, analysed by Gas Chromatography–Flame Ionization Detector (GC-FID) and Gas Chromatography-Mass Spectrometry (GC-MS) analyses, at different times. Moreover, considering the role of free radicals in the progression of neurodegenerative disorders, the antioxidant properties of essential oils were investigated by using, 2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and β-carotene bleaching tests. The relative antioxidant capacity index (RACI) was used to achieve more comprehensive comparison between analysed antioxidant effects of essential oils. P. armeniaca oils were more active than P. domestica oils against AChE. Against BChE, the most active was the essential oil from P. domestica leaves collected in August with an IC50 value of 95.80 μg/mL. This oil exerted the highest inhibitory activity of lipid peroxidation with IC50 values of 11.15 and 11.39 μg/mL after 30 and 60 min of incubation, respectively. All samples demonstrated a remarkable ABTS radicals scavenging activity, with IC50 values in the range 0.45–0.57 μg/mL in comparison to the positive control, ascorbic acid.

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